1933460-18-4
Chemical Structure
(rac)-Mitiperstat
Synonym(s): (rac)-AZD4831
- CAS. Nr.: 1933460-18-4
- Formula:C15H15ClN4OS
- Molecular Weight:334.82
InChIKey: BHKKSKOHRFHHIN-UHFFFAOYSA-N
SMILES: O=C(NC1=S)C(NC=C2)=C2N1CC3=C(C=C(C=C3)Cl)C(N)C
Biological Activity: (rac)-Mitiperstat ((rac)-AZD4831) is the racemic form of Mitiperstat (HY-145581). Mitiperstat (AZD4831) is an effective oral inhibitor of myeloperoxidase (MPO). Mitiperstat inhibits MPO and thyroid peroxidase (TPO) with IC50s of 1.5 nM and 0.69 μM. Mitiperstat exhibits a weak inhibitory activity against CYP3A4 with an IC50 of 6 μM. Mitiperstat can reduce inflammation and improve microvascular function, and it can be used in studies related to heart failure, preserved or mildly reduced ejection fraction, non-alcoholic fatty liver disease, and chronic obstructive pulmonary disease[1][2][3][4].
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(rac)-Mitiperstat | 98.25% | (rac)-Mitiperstat ((rac)-AZD4831) is the racemic form of Mitiperstat (HY-145581). Mitiperstat (AZD4831) is an effective oral inhibitor of myeloperoxidase (MPO). Mitiperstat inhibits MPO and thyroid peroxidase (TPO) with IC50s of 1.5 nM and 0.69 μM. Mitiperstat exhibits a weak inhibitory activity against CYP3A4 with an IC50 of 6 μM. Mitiperstat can reduce inflammation and improve microvascular function, and it can be used in studies related to heart failure, preserved or mildly reduced ejection fraction, non-alcoholic fatty liver disease, and chronic obstructive pulmonary disease. | ||||||||||||||||||||
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- [1]. Joanna Parkinson， et al. The myeloperoxidase inhibitor mitiperstat (AZD4831) does not prolong the QT interval at expected therapeutic doses. Pharmacol Res Perspect. 2024 Apr;12(2):e1184. [Content Brief]
- [2]. Lars H Lund, et al. Rationale and design of ENDEAVOR: A sequential phase 2b-3 randomized clinical trial to evaluate the effect of myeloperoxidase inhibition on symptoms and exercise capacity in heart failure with preserved or mildly reduced ejection fraction. Eur J Heart Fail. 2023 Sep;25(9):1696-1707. [Content Brief]
- [3]. Carolyn S P Lam, et al. Myeloperoxidase Inhibition in Heart Failure With Preserved or Mildly Reduced Ejection Fraction: SATELLITE Trial Results. J Card Fail. 2024 Jan;30(1):104-110. [Content Brief]
- [4]. Inghardt T, et al., Discovery of AZD4831, a Mechanism-Based Irreversible Inhibitor of Myeloperoxidase, As a Potential Treatment for Heart Failure with Preserved Ejection Fraction. J Med Chem. 2022 Sep 8;65(17):11485-11496. [Content Brief]
Keywords
